Assay Detail
Binding
CHEMBL972582
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Inhibition of DNA-dependent protein kinase
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
DNA-dependent protein kinase catalytic subunit (CHEMBL3142) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
8-Biarylchromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 49 | 6.26 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL188678 | — | — | 1 | 7.92 |
| CHEMBL529223 | — | — | 1 | 7.75 |
| CHEMBL488881 | — | — | 1 | 7.70 |
| CHEMBL454422 | — | — | 1 | 7.05 |
| CHEMBL508479 | — | — | 1 | 7.05 |
| CHEMBL471335 | — | — | 1 | 6.85 |
| CHEMBL454660 | — | — | 1 | 6.77 |
| CHEMBL512322 | — | — | 1 | 6.75 |
| CHEMBL462199 | — | — | 1 | 6.62 |
| CHEMBL508976 | — | — | 1 | 6.62 |
| CHEMBL488880 | — | — | 1 | 6.58 |
| CHEMBL487033 | — | — | 1 | 6.57 |
| CHEMBL460952 | — | — | 1 | 6.52 |
| CHEMBL453884 | — | — | 1 | 6.47 |
| CHEMBL521403 | — | — | 1 | 6.44 |
| CHEMBL454658 | — | — | 1 | 6.43 |
| CHEMBL487032 | — | — | 1 | 6.42 |
| CHEMBL454423 | — | — | 1 | 6.40 |
| CHEMBL454659 | — | — | 1 | 6.32 |
| CHEMBL488903 | — | — | 1 | 6.31 |
| CHEMBL503589 | — | — | 1 | 6.29 |
| CHEMBL486876 | — | — | 1 | 6.29 |
| CHEMBL518820 | — | — | 1 | 6.29 |
| CHEMBL462200 | — | — | 1 | 6.21 |
| CHEMBL488213 | — | — | 1 | 6.19 |
| CHEMBL452577 | — | — | 1 | 6.17 |
| CHEMBL454429 | — | — | 1 | 6.15 |
| CHEMBL513231 | — | — | 1 | 6.08 |
| CHEMBL529668 | — | — | 1 | 6.06 |
| CHEMBL488023 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL188678 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL529223 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL488881 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL454422 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL508479 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL471335 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL454660 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL512322 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL462199 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL508976 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL488880 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL487033 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL460952 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL453884 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL521403 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL454658 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL487032 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL454423 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL454659 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL488903 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL503589 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL486876 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL518820 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL462200 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL488213 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL452577 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL454429 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL513231 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL529668 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL488023 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL488882 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL519754 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL488212 | — | IC50 | = | 1130.0 | nM | 5.95 |
| CHEMBL488893 | — | IC50 | = | 1230.0 | nM | 5.91 |
| CHEMBL460953 | — | IC50 | = | 1240.0 | nM | 5.91 |
| CHEMBL459887 | — | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL462008 | — | IC50 | = | 1410.0 | nM | 5.85 |
| CHEMBL471336 | — | IC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL509606 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL98350 | LY-294002 | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL453889 | — | IC50 | = | 1570.0 | nM | 5.80 |
| CHEMBL518667 | — | IC50 | = | 1750.0 | nM | 5.76 |
| CHEMBL529898 | — | IC50 | = | 1820.0 | nM | 5.74 |
| CHEMBL488024 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL517898 | — | IC50 | = | 2370.0 | nM | 5.62 |
| CHEMBL453883 | — | IC50 | = | 2460.0 | nM | 5.61 |
| CHEMBL453888 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL488892 | — | IC50 | = | 3010.0 | nM | 5.52 |
| CHEMBL462201 | — | IC50 | = | 4450.0 | nM | 5.35 |